ChemicalBook > CAS DataBase List > 1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide

1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide

Product Name
1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide
CAS No.
1396772-26-1
Chemical Name
1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide
Synonyms
CS-724;EPZ 00568;EPZ005687;EPZ-005687;EPZ 00568;EPZ005687;EPZ-005687;1-Cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)ph;1-CYCLOPENTYL-N-((4,6-DIMETHYL-2-OXO-1,2-DIHYDROPYRIDIN-3-YL)METHYL)-6-(4-(MORPHOLINOMETHYL)PHENYL)-;1-cyclopentyl-n-[(4,6-dimethyl-2-oxo-1h-pyridin-3-yl)methyl]-6-[4-(morpholin-4-ylmethyl)phenyl]indazole-4-carboxamide;1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide;1H-Indazole-4-carboxamide, 1-cyclopentyl-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-6-[4-(4-morpholinylmethyl)phenyl]-
CBNumber
CB02645672
Molecular Formula
C32H37N5O3
Formula Weight
539.67
MOL File
1396772-26-1.mol
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1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide Property

Boiling point:
797.9±60.0 °C(Predicted)
Density 
1.31±0.1 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
insoluble in EtOH; insoluble in H2O; ≥3.86 mg/mL in DMSO
form 
solid
pka
11.88±0.10(Predicted)
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Cayman Chemical
Product number
13966
Product name
EPZ005687
Purity
≥98%
Packaging
5mg
Price
$86
Updated
2024/03/01
Cayman Chemical
Product number
13966
Product name
EPZ005687
Purity
≥98%
Packaging
10mg
Price
$152
Updated
2024/03/01
Cayman Chemical
Product number
13966
Product name
EPZ005687
Purity
≥98%
Packaging
25mg
Price
$336
Updated
2024/03/01
Cayman Chemical
Product number
13966
Product name
EPZ005687
Purity
≥98%
Packaging
50mg
Price
$588
Updated
2024/03/01
TRC
Product number
E592200
Product name
EPZ005687
Packaging
5mg
Price
$275
Updated
2021/12/16
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1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide Chemical Properties,Usage,Production

Uses

EPZ005687 is a potent, selective inhibitor of the lysine methyltranferase EZH2 (Ki = 24 nM), the enzymatic subunit of polycomb repressive complex 2 (PRC2). It acts competitively with the EZH2 substrate S-adenosylmethionine. EPZ005687 has greater than 500-fold selectivity against 15 other protein methyltransferases and has 50-fold selectivity against EZH1. It blocks trimethylation of the PRC2 target histone 3 lysine 27 (IC50 = 80 nM), decreasing the proliferation of lymphoma cells carrying mutant, but not wild-type, EZH2.[Cayman Chemical]

Uses

EPZ005687 is a potent and selective inhibitor of EZH2.

Definition

ChEBI: 1-cyclopentyl-N-[(4,6-dimethyl-2-oxo-1H-pyridin-3-yl)methyl]-6-[4-(4-morpholinylmethyl)phenyl]-4-indazolecarboxamide is a member of indazoles.

Biological Activity

epz005687 is a potent inhibitor of ezh2, an enzymatic subunit of polycomb repressive complex 2 (prc2) catalyzing the methylation of histone h3 lysine 27 (h3k27), that inhibits ezh2 with a value of inhibition constant ki of 24 nm, which is 500-fold and 50-fold greater in selectivity than 15 other protein methyltransferases and closely related ezh1 respectively. epz005687 concentration-dependently inhibits the enzymatic activity of prc2 with a value of 50% inhibition concentration ic50 of 54 nm through binding to the s-adenosylmethionine (sam) pocket of the ezh2 set domain. study results have shown that epz005687 reduces h3k27 methylation in a variety of lymphoma cells and induces apoptotic cell killing in heterozygous tyr641 or ala677 mutant cells.knutson sk, wigle tj, warholic nm, sneeringer cj, allain cj, klaus cr, sacks jd, raimondi a, majer cr, song j, scott mp, jin l, smith jj, olhava ej, chesworth r, moyer mp, richon vm, copeland ra, keilhack h, pollock rm, kuntz kw. a selective inhibitor of ezh2 blocks h3k27 methylation and kills mutant lymphoma cells. nat chem biol. 2012 nov;8(11):890-6.

target

EZH2

1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide Preparation Products And Raw materials

Raw materials

Preparation Products

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1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide Suppliers

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View Lastest Price from 1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide manufacturers

Career Henan Chemical Co
Product
1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide 1396772-26-1
Price
US $1.00-1.00/KG
Min. Order
1KG
Purity
98%
Supply Ability
1lg; 2kg; 5kg; 10kg; 100kg
Release date
2019-08-31

1396772-26-1, 1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMideRelated Search:


  • EPZ005687;EPZ-005687
  • 1-Cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)ph
  • 1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide
  • EPZ005687
  • 1H-Indazole-4-carboxamide, 1-cyclopentyl-N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-6-[4-(4-morpholinylmethyl)phenyl]-
  • 1-Cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide EPZ 005687
  • EPZ 005687 1-Cyclopentyl-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-6-(4-(morpholinomethyl)phenyl)-1H-indazole-4-carboxamide
  • EPZ 00568
  • EPZ-005687;EPZ 00568
  • CS-724
  • 1-CYCLOPENTYL-N-((4,6-DIMETHYL-2-OXO-1,2-DIHYDROPYRIDIN-3-YL)METHYL)-6-(4-(MORPHOLINOMETHYL)PHENYL)-
  • 1-cyclopentyl-n-[(4,6-dimethyl-2-oxo-1h-pyridin-3-yl)methyl]-6-[4-(morpholin-4-ylmethyl)phenyl]indazole-4-carboxamide
  • 1-Cyclopentyl-N-((4,6-diMethyl-2-oxo-1,2-dihydropyridin-3-yl)Methyl)-6-(4-(MorpholinoMethyl)phenyl)-1H-indazole-4-carboxaMide USP/EP/BP
  • 1396772-26-1
  • C32H37N5O3
  • Inhibitors
  • API